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Assay Detail

CHEMBL4822202

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant human N-terminal Flag-tagged TET1 (1418 to 2136 residues) expressed in Baculovirus infected Sf9 cells assessed as reduction in 5hmc level incubated for 2 hrs by ELISA
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Methylcytosine dioxygenase TET1 (CHEMBL4523402)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR insights into TET2 catalytic domain inhibition: Synthesis of 2-Hydroxy-4-Methylene-pentanedicarboxylates.
Tiwari AD, Guan Y, Grabowski DR, Maciejewski JP, Jha BK, Phillips JG.
Bioorg Med Chem (2021) 39 : 116141 -116141
PubMed 33894507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.82 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4851104 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4851104 IC50 = 1500.0 nM 5.82